Baboota S, Al-Azaki A, Kohli K, Ali J, Dixit N, Shakeel F
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi-1100 62, India.
PDA J Pharm Sci Technol. 2007 Jul-Aug;61(4):276-85.
The aim of the present study is to develop and evaluate microemulsion formulations for Terbinafine (TB) with a view to enhance its permeability through the skin and provide release for 24 h. Various o/w microemulsions were prepared by the spontaneous emulsification method. Oleic acid was chosen as the oil phase, Caprylo caproyl macrogol-8- glyceride (Labrasol S) and purified diethylene glycol monoethyl ether (Transcutol P) were used as surfactant and cosurfactant, respectively, on the basis of solubility studies. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, cosurfactant, and water for microemulsion formulation. The optimized microemulsion consisted of 2% w/w TB, 8% w/w oleic acid, 31% w/w labrasol S, 31% w/w transcutol P, and 30% w/w distilled water. Permeability parameters like Jss and Kp were found to be significantly higher for formulation F4 as compared to other formulations (P < 0.05). Microbiological studies of TB in microemulsion showed better anti-fungal activity against Candida albicans and Aspergillus flavus as compared to marketed product (P < 0.05).
本研究的目的是开发并评估特比萘芬(TB)的微乳剂配方,以提高其经皮渗透性并实现24小时释放。通过自发乳化法制备了各种油包水型微乳剂。基于溶解度研究,选择油酸作为油相,辛酰己酰聚乙二醇-8-甘油酯(Labrasol S)和纯化的二甘醇单乙醚(Transcutol P)分别用作表面活性剂和助表面活性剂。构建伪三元相图以获得微乳剂配方中油、表面活性剂、助表面活性剂和水的浓度范围。优化后的微乳剂由2%(w/w)的TB、8%(w/w)的油酸、31%(w/w)的Labrasol S、31%(w/w)的Transcutol P和30%(w/w)的蒸馏水组成。与其他配方相比,发现配方F4的渗透参数如稳态通量(Jss)和渗透系数(Kp)显著更高(P < 0.05)。微乳剂中TB的微生物学研究表明,与市售产品相比,其对白色念珠菌和黄曲霉具有更好的抗真菌活性(P < 0.05)。